Target Information
| Target General Information | Top | |||||
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| Target ID |
T45674
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| Target Name |
Sigma intracellular receptor 2 (TMEM97)
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| Synonyms |
Transmembrane protein 97; Sigma2 receptor; Sigma-2 receptor; Meningioma-associated protein 30; MAC30
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| Gene Name |
TMEM97
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Schizophrenia [ICD-11: 6A20] | |||||
| Function |
Intracellular orphan receptor that binds numerous drugs and which is highly expressed in various proliferating cancer cells. Corresponds to the sigma-2 receptor, which is thought to play important role in regulating cell survival, morphology and differentiation. Under investigation for its potential diagnostic and therapeutic uses. May play a role as a regulator of cellular cholesterol homeostasis. May function as sterol isomerase. May alter the activity of some cytochrome P450 proteins.
Click to Show/Hide
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| BioChemical Class |
TMEM97/sigma-2 receptor
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| UniProt ID | ||||||
| Sequence |
MGAPATRRCVEWLLGLYFLSHIPITLFMDLQAVLPRELYPVEFRNLLKWYAKEFKDPLLQ
EPPAWFKSFLFCELVFQLPFFPIATYAFLKGSCKWIRTPAIIYSVHTMTTLIPILSTFLF EDFSKASGFKGQRPETLHERLTLVSVYAPYLLIPFILLIFMLRSPYYKYEEKRKKK Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| Drugs and Modes of Action | Top | |||||
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| Clinical Trial Drug(s) | [+] 2 Clinical Trial Drugs | + | ||||
| 1 | MIN-101 | Drug Info | Phase 3 | Schizophrenia | [2] | |
| 2 | CT1812 | Drug Info | Phase 2 | Alzheimer disease | [3] | |
| Preclinical Drug(s) | [+] 1 Preclinical Drugs | + | ||||
| 1 | ANAVEX 1007 | Drug Info | Preclinical | Pancreatic cancer | [4] | |
| Mode of Action | [+] 3 Modes of Action | + | ||||
| Antagonist | [+] 3 Antagonist drugs | + | ||||
| 1 | MIN-101 | Drug Info | [1] | |||
| 2 | CT1812 | Drug Info | [5], [6] | |||
| 3 | SM 21 | Drug Info | [11] | |||
| Ligand | [+] 52 Ligand drugs | + | ||||
| 1 | Aryl azepine derivative 1 | Drug Info | [7] | |||
| 2 | Aryl azepine derivative 2 | Drug Info | [7] | |||
| 3 | Benzamide derivative 1 | Drug Info | [8] | |||
| 4 | Benzamide derivative 10 | Drug Info | [7] | |||
| 5 | Benzamide derivative 11 | Drug Info | [7] | |||
| 6 | Benzamide derivative 2 | Drug Info | [8] | |||
| 7 | Benzamide derivative 3 | Drug Info | [8] | |||
| 8 | Benzamide derivative 4 | Drug Info | [8] | |||
| 9 | Benzamide derivative 7 | Drug Info | [7] | |||
| 10 | Benzamide derivative 8 | Drug Info | [7] | |||
| 11 | Benzamide derivative 9 | Drug Info | [7] | |||
| 12 | Bicyclo-heptan-2-amine derivative 1 | Drug Info | [8] | |||
| 13 | Bicyclo-heptan-2-amine derivative 2 | Drug Info | [8] | |||
| 14 | Bicyclo-heptan-2-amine derivative 3 | Drug Info | [8] | |||
| 15 | Bicyclo-heptan-2-amine derivative 4 | Drug Info | [8] | |||
| 16 | Fused aryl carbocycle derivative 1 | Drug Info | [7] | |||
| 17 | Fused aryl carbocycle derivative 2 | Drug Info | [7] | |||
| 18 | Fused aryl carbocycle derivative 3 | Drug Info | [7] | |||
| 19 | Fused aryl carbocycle derivative 4 | Drug Info | [7] | |||
| 20 | Fused aryl carbocycle derivative 8 | Drug Info | [7] | |||
| 21 | Fused aryl carbocycle derivative 9 | Drug Info | [7] | |||
| 22 | Isoindoline derivative 1 | Drug Info | [7] | |||
| 23 | Isoindoline derivative 2 | Drug Info | [7] | |||
| 24 | Isoindoline derivative 3 | Drug Info | [7] | |||
| 25 | Isoindoline derivative 4 | Drug Info | [7] | |||
| 26 | Isoindoline derivative 5 | Drug Info | [7] | |||
| 27 | N-substituted 9-azabicyclo[3.3.1]nonan-3alpha-yl-phenylcarbamate analog 1 | Drug Info | [8] | |||
| 28 | N-substituted 9-azabicyclo[3.3.1]nonan-3alpha-yl-phenylcarbamate analog 2 | Drug Info | [8] | |||
| 29 | N-substituted 9-azabicyclo[3.3.1]nonan-3alpha-yl-phenylcarbamate analog 3 | Drug Info | [8] | |||
| 30 | Piperazine derivative 7 | Drug Info | [8] | |||
| 31 | Piperazinyl methyl quinazolinone derivative 1 | Drug Info | [7] | |||
| 32 | Piperazinyl methyl quinazolinone derivative 2 | Drug Info | [7] | |||
| 33 | Piperazinyl methyl quinazolinone derivative 3 | Drug Info | [7] | |||
| 34 | Piperazinyl norbenzomorphane compound 1 | Drug Info | [7] | |||
| 35 | Piperazinyl norbenzomorphane compound 2 | Drug Info | [7] | |||
| 36 | Piperazinyl norbenzomorphane compound 3 | Drug Info | [7] | |||
| 37 | Piperazinyl norbenzomorphane compound 4 | Drug Info | [7] | |||
| 38 | Piperidine derivative 5 | Drug Info | [8] | |||
| 39 | Piperidine derivative 6 | Drug Info | [8] | |||
| 40 | PMID28051882-Compound-Figure9 | Drug Info | [8] | |||
| 41 | PMID28051882-Compound-XI | Drug Info | [8] | |||
| 42 | PMID28051882-Compound-XIV | Drug Info | [8] | |||
| 43 | PMID30185082-Compound-14 | Drug Info | [7] | |||
| 44 | PMID30185082-Compound-27 | Drug Info | [7] | |||
| 45 | PMID30185082-Compound-28 | Drug Info | [7] | |||
| 46 | PMID30185082-Compound-53 | Drug Info | [7] | |||
| 47 | PMID30185082-Compound-54 | Drug Info | [7] | |||
| 48 | PMID30185082-Compound-55 | Drug Info | [7] | |||
| 49 | PMID30185082-Compound-56 | Drug Info | [7] | |||
| 50 | PMID30185082-Compound-57 | Drug Info | [7] | |||
| 51 | PMID30185082-Compound-63 | Drug Info | [7] | |||
| 52 | PMID30185082-Compound-64 | Drug Info | [7] | |||
| Agonist | [+] 2 Agonist drugs | + | ||||
| 1 | ANAVEX 1007 | Drug Info | [4] | |||
| 2 | 1,3-ditolylguanidine | Drug Info | [9], [10] | |||
| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 2 | ClinicalTrials.gov (NCT03397134) Study to Evaluate Efficacy and Safety of Roluperidone (MIN-101) in Adult Patients With Negative Symptoms of Schizophrenia. U.S. National Institutes of Health. | |||||
| REF 3 | ClinicalTrials.gov (NCT04735536) Pilot Clinical Study of CT1812 in Mild to Moderate Alzheimer's Disease Using EEG. U.S. National Institutes of Health. | |||||
| REF 4 | 2011 Pipeline of Anavex. | |||||
| REF 5 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 6 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 7 | The sigma-2 (-2) receptor: a review of recent patent applications: 2013-2018.Expert Opin Ther Pat. 2018 Sep;28(9):655-663. | |||||
| REF 8 | Are sigma modulators an effective opportunity for cancer treatment A patent overview (1996-2016).Expert Opin Ther Pat. 2017 May;27(5):565-578. | |||||
| REF 9 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2553). | |||||
| REF 10 | Sigma1 and sigma2 receptor binding affinity and selectivity of SA4503 and fluoroethyl SA4503. Synapse. 2006 May;59(6):350-8. | |||||
| REF 11 | The analgesic tropane analogue (+/-)-SM 21 has a high affinity for sigma2 receptors. Life Sci. 1999;64(10):PL131-7. | |||||
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